Ospemifene: New treatment for postmenopausal women

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April 01, 2013

Osphena (ospemifene—Shionogi)

A new once-daily oral tablet, ospemifene (Osphena—Shionogi), has received FDA approval for treating moderate to severe dyspareunia in postmenopausal women. Dyspareunia is a condition characterized by pain during sexual intercourse and usually is a symptom of vulvar and vaginal atrophy due to menopause.

Ospemifene is an estrogen agonist/antagonist that makes vaginal tissue thicker and less fragile, resulting in a reduction in the amount of pain women experience with sexual intercourse.

This new therapy is recommended to be used for the shortest duration with consideration given to treatment goals and potential risks. The labeling states that women should be reevaluated periodically, as clinically appropriate, to determine if treatment is still necessary.

Management of vulvovaginal atrophy–related sexual dysfunction

Sexual dysfunction has been reported as a common problem among postmenopausal women, with nearly three-quarters of women older than 60 years reporting sexual inactivity, difficulty with intercourse, or dyspareunia. These symptoms contribute to the hypoestrogenic state of postmenopausal women. Vulvar atrophy and vulvar lesions may be observed upon examination, which contribute to the dyspareunia.

Traditionally, management of vulvovaginal atrophy–related sexual dysfunction has focused on the use of oral, transdermal, or vaginal estrogen preparations. Vaginal estrogen preparations with the lowest systemic absorption rate are generally preferred for women who present solely with vaginal symptoms and no other postmenopausal complaints (e.g., hot flashes). Vaginal lubricants and moisturizers applied regularly are also options for women who want to avoid the use of estrogen altogether. Approval of ospemifene now offers women yet another treatment option to help them deal with this condition.

Clinical data

Approval was based on data from three placebo-controlled studies involving 1,889 postmenopausal women with symptoms of vulvar and vaginal atrophy who were randomly assigned to receive ospemifene (n = 1,102) or a placebo (n = 787). After 12 weeks of treatment, results from the first two trials showed a statistically significant improvement in dyspareunia among women treated with ospemifene compared with placebo. Results from the third study supported the drug’s long-term safety in treating dyspareunia. Common adverse effects reported during clinical trials included hot flushes/flashes, vaginal discharge, muscle spasms, genital discharge, and excessive sweating.

Ospemifene was approved with a boxed warning alerting women and health professionals that the drug has been shown to stimulate the endometrium and cause it to thicken (see sidebar). The boxed warning also includes an alert about estrogen therapies increasing the risk of stroke and deep vein thrombosis. The incidence rates of thrombotic and hemorrhagic strokes with ospemifene were reported to be 0.72 and 1.45 per 1,000 women, respectively, compared with 1.04 and 0 per 1,000 women for placebo, and the incidence rate of deep vein thrombosis was reported to be 1.45 per 1,000 women compared with 1.04 per 1,000 women for placebo.

Ospemifene (Osphena)

Manufacturer: Shionogi

Drug class: Estrogen agonist/antagonist

Indication: Treatment of moderate to severe dyspareunia

Dosage: One 60-mg tablet taken orally once daily with food

Of note: Ospemifene has a boxed warning describing the potential for endometrial cancer and cardiovascular disorders (e.g., stroke, coronary heart disease, venous thromboembolism), as well as increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adding a progestin reduces the risk of endometrial hyperplasia.

The drug is contraindicated in women with undiagnosed abnormal genital bleeding; known or suspected estrogen-dependent neoplasia; active or history of deep vein thrombosis, pulmonary embolism, or arterial thromboembolic disease; and who are or may become pregnant.

Ospemifene should not be used in women with known or suspected breast cancer or those with severe hepatic impairment.

Patient counseling

Give patients the FDA-approved Patient Information sheet and educate them on proper use and potential adverse reactions. Inform patients that the tablets should be taken once daily with food and that continued use of ospemifene should be discussed with their provider regularly (i.e., every 3 to 6 mo) to determine if treatment is still needed. Review common adverse reactions (e.g., hot flashes, excessive sweating) and more serious events (e.g., blood clots).